2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. CYP1B1-IN-9

CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance.

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CYP1B1-IN-9 Chemical Structure

CYP1B1-IN-9 Chemical Structure

CAS No. : 3077254-39-5

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CYP1B1-IN-9 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance[1].
In Vitro

CYP1B1-IN-9 (Compound B20) (15-45 min) exhibits the IC50 values of >100 (CYP1A1) and >80 (CYP1A2), and the inhibition rates of CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 are 15.7%, 2.21%, 7.73%, 0.0% and 0.940%, respectively[1].
CYP1B1-IN-9 (20, 40 μM, 48 h) exhibits low cytotoxicity (IC50 HUVEC > 40 μM; IC50 BEAS 2B > 20 μM) and sensitivity in A549/T cells with an IC50 of 7.5 μM[1].
CYP1B1-IN-9 (2.5 μM, 48 h) has strong synergistic effects with Paclitaxel (0.025 μM, CI = 0.08), confirming the ability to reverse multidrug resistance through CYP1B1 inhibition[1].
CYP1B1-IN-9 (2.5-10 μM, 24 h) concentration-dependently suppressed A549/T cell migration[1].
CYP1B1-IN-9 (5-60 min, 0.5 mg/mL) has superior metabolic stability with half-lives (T1/2) of exceeding 60 min and intrinsic clearance rates (CLint) of 1.1 mL/min/kg in vitro liver microsomal studies[1].
CYP1B1-IN-9 (5-120 min, 100 μM) has human plasma stability with T1/2 values surpassing 2 h[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CYP1B1-IN-9 Related Antibodies

Cell Migration Assay [1]

Cell Line: A549/T cells
Concentration: 2.5, 5.0, 10 μM
Incubation Time: 24 h
Result: Suppressed concentration-dependently cell migration, achieving 3% wound closure at 5.0 μM compared to 12.6% for TMS at the same concentration.
Reduced invasive cells to 35.7% of control at 2.5 μM, outperforming TMS (40.2% at 5.0μM).
Parmacokinetics
Species Dose Route Indicator value
Rat 10 mg/kg p.o. T1/2 1.12 h
Rat 2 mg/kg i.v. T1/2 3.78 h
Rat 10 mg/kg p.o. Tmax 1.00 h
Rat 2 mg/kg i.v. Tmax 0.08 h
Rat 10 mg/kg p.o. AUC0-t 236 ng·h/mL
Rat 2 mg/kg i.v. Cmax 4750 ng/mL
Rat 10 mg/kg p.o. AUC0-∞ 239 ng·h/mL
Rat 2 mg/kg i.v. AUC0-t 2292 ng·h/mL
Rat 10 mg/kg p.o. MRT0-t 2.32 h
Rat 2 mg/kg i.v. AUC0-∞ 2302 ng·h/mL
Rat 10 mg/kg p.o. MRT0-∞ 2.42 h
Rat 2 mg/kg i.v. MRT0-t 0.64 h
Rat 10 mg/kg p.o. F 2.08 %
Rat 2 mg/kg i.v. MRT0-∞ 0.73 h
Rat 10 mg/kg p.o. Cmax 81.0 mL/kg
Rat 2 mg/kg i.v. CL 883 mL/h/kg
Rat 2 mg/kg i.v. Vz 4766 mg/L
Molecular Weight

383.68

Formula

C16H9Cl3N2OS
CAS No.
SMILES

O=C(C1=NC(C2=CC=CC(Cl)=C2)=CS1)NC3=CC(Cl)=CC(Cl)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CYP1B1-IN-9 Related Classifications

  • Molarity Calculator

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CYP1B1-IN-93077254-39-5Cytochrome P450CYPsTumor-drug resistanceA549/TRatPaclitaxelCYPInhibitorinhibitorinhibit

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